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Preparation method of ferroferric oxide surface double-modified adriamycin targeted drug

A technology of ferric tetroxide and doxorubicin is applied in the field of preparation of doxorubicin-targeted drugs, which can solve problems such as insufficient sensitivity, and achieve the effects of overcoming drug resistance, rational reaction design, and reducing toxic and side effects.

Active Publication Date: 2017-05-17
NINGBO UNIV
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the doxorubicin magnetic targeting drug also has chitosan-polyethylene glycol Fe 3 o 4 The surface is double-modified, but the sensitivity is insufficient, because there is a significant difference between the acidic environment of the tumor site and the normal tissue (the pH value of the normal tissue is generally about 7.4, while the pH value of the tumor site is 4.5~6.0), the magnetic targeting and the A combination of acid-sensitive dual mechanisms of action, such dual targeting mechanisms, Fe 3 o 4 As the magnetic targeting site, nanoparticles have the function of magnetron guidance. They reach the lesion through the external magnetic field orientation and concentrate in the tumor site. The acidic environment of the tumor also promotes the breakage of the hydrazone bond, thereby releasing the drug, overcoming the drug resistance of the tumor, and reducing the risk of cancer. Toxic side effects of chemotherapy drugs

Method used

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Experimental program
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Effect test

Embodiment 1

[0011] Measure 5~10mL of ammonia water and 2~5mL of hydrazine hydrate, and dissolve 50~70mL of deionized water in a three-neck bottle, raise the temperature to 80~100°C, and weigh 1~2g of FeCl 2 4H 2 O and 2~3g FeCl 3 ·6H 2 O, dissolved in 20~30mL water, added to a three-necked bottle to form a reaction solution system to react until the solution system turns black, stir vigorously at 80~95°C for 30~60min, and then stir when the pH of the solution is 9~10 Add 10~20mL of citric acid with a concentration of 0.3g / mL dropwise, and continue to stir for 1.5~2 h after the dropwise addition. After cooling to room temperature, use an external strong magnet to collect the black product, and wash the obtained product with a mixture of deionized water and acetone several times to remove the unreacted citric acid, and vacuum-dry the black product at 30-50°C for 12-24 hours to obtain citric acid-modified ferric oxide (Fe 3 o 4 )Nanoparticles. Take 5~10g of citric acid-modified ferrofer...

Embodiment 2

[0013] Precisely weigh Fe with maximum drug loading rate 3 o 4 The surface double-modified doxorubicin targeted drug was properly dispersed in PBS buffer solution with pH=7.4, the solution volume was 2-4 mL, placed in a dialysis bag, and put into a brown vial containing 8-10 mL, 37 10 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, 24 h, 48 h, and 72 h were sampled 1-2 mL for in vitro release investigation, and the same volume of fresh Release the medium, take the supernatant to measure the UV absorbance value, and calculate the cumulative drug release rate. The result is that the release rate of doxorubicin under the condition of pH=5 is higher than that under the condition of pH=7.4, which are 78% and 27%, respectively, and has obvious pH sensitivity and good slow-release performance.

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Abstract

The invention discloses a preparation method of a Fe3O4 surface double-modified adriamycin targeted drug. The preparation method comprises the following steps: firstly by taking FeCl2.4H2O, FeCl3.6H2O and citric acid as raw materials, reacting and drying to obtain citric acid modified Fe3O4 nano particles by taking ammonium hydroxide, hydrazine hydrate and water as a reaction medium, and then reacting with dicarboxylate polyethylene glycol under the effect of a coupling agent and hydrazine hydrate, drying to obtain the citric acid / polyethylene glycol double-modified ferroferric oxide nano particles, reacting with adriamycin in a methanol solution, drying to obtain the Fe3O4 surface double-modified adriamycin targeted drug. The invention provides the preparation method of Fe3O4 surface double-modified adriamycin targeted drug with the drug sustained release behavior in good superparamagnetism and acid sensitivity.

Description

technical field [0001] The present invention relates to the preparation of doxorubicin targeting drug, in particular to a kind of Fe 3 o 4 The preparation method of the double-modified doxorubicin targeting drug. Background technique [0002] Magnetic drug targeting (MDT) can guide the magnetism of magnetic nanoparticles through an external magnetic field, improve the efficiency of chemotherapy drugs reaching the lesion site, and enhance targeting. Doxorubicin-targeted drugs are targeted drugs targeting tumor cells, which can reduce the toxic and side effects of chemotherapy drugs on normal cells. Fe 3 o 4 Chemical substances for surface modification of magnetic nanoparticles include: citric acid, polyethylene glycol, chitosan, polyaniline, polysorbate and other small organic molecules or high molecular compounds, as well as inorganic compounds such as gold, carbon and silicon dioxide. Among them, polyethylene glycol (PEG) has been approved for use by the US Food and Dr...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K31/704A61P35/00
Inventor 季帆张剑锋张坤张婷婷
Owner NINGBO UNIV
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